The study analyzed that the BET inhibitors pipeline comprised 38 drug candidates in different stages of development.

Insights on pipeline segments

As per the findings of the research, most of the BET inhibitor pipeline drug candidates are being developed to be administered by oral route.

IC50 value and Kd of different types of BET inhibitors

In BET inhibitors, IC50 value is measured as the concentration of drug at which 50% of the target is inhibited. IC50 is a pharmacokinetic measure; the lower the IC50 of drug candidate, the lesser the desired effect, and the less likelihood of the drug to have some off-target effect. Kd is known as dissociation constant of drug. It measures the rate of dissociation of the drug and its binding affinity. Birabresib (MK8628), a BET inhibitor by Merck & Co., has IC50 value of 100nM.

Strategic collaborations for the development of BET inhibitors

The research finds that different companies are collaborating for the development of BET inhibitors. In January 2017, ConverGene had entered into a sponsored research agreement with the University of Maryland, Baltimore to investigate the in vivo anti-leukemic effects of ConverGene’s lead BET inhibitor drug candidates, CG223 and CG250.